{"title":"Chemical Synthesis of the Anti-COVID-19 Drug Remdesivir.","authors":"Mo Wang, Lu Zhang, Xiaohong Huo, Zhenfeng Zhang, Wanbin Zhang","doi":"10.1002/cpz1.303","DOIUrl":null,"url":null,"abstract":"<p><p>Remdesivir has become an important compound for the treatment of COVID-19. Here, we describe the catalytic asymmetric synthesis of this anti-COVID-19 drug. First, the P-racemic phosphoryl chloride is synthesized in a facile procedure. Then, it is possible to obtain the protected remdesivir via the organocatalytic asymmetric phosphorylation of protected nucleoside GS441524 with P-racemic phosphoryl chloride catalyzed by chiral bicyclic imidazole. Finally, remdesivir is easily prepared by deprotection. © 2021 Wiley Periodicals LLC. Basic Protocol 1: Synthesis of 2-ethylbutyl (chloro(phenoxy)phosphoryl)-L-alaninate rac-4 Basic Protocol 2: Synthesis of chiral bicyclic imidazole Ad-DPI Basic Protocol 3: Synthesis of remdesivir.</p>","PeriodicalId":11174,"journal":{"name":"Current Protocols","volume":" ","pages":"e303"},"PeriodicalIF":0.0000,"publicationDate":"2021-12-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9015308/pdf/CPZ1-1-e303.pdf","citationCount":"2","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Current Protocols","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.1002/cpz1.303","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 2
Abstract
Remdesivir has become an important compound for the treatment of COVID-19. Here, we describe the catalytic asymmetric synthesis of this anti-COVID-19 drug. First, the P-racemic phosphoryl chloride is synthesized in a facile procedure. Then, it is possible to obtain the protected remdesivir via the organocatalytic asymmetric phosphorylation of protected nucleoside GS441524 with P-racemic phosphoryl chloride catalyzed by chiral bicyclic imidazole. Finally, remdesivir is easily prepared by deprotection. © 2021 Wiley Periodicals LLC. Basic Protocol 1: Synthesis of 2-ethylbutyl (chloro(phenoxy)phosphoryl)-L-alaninate rac-4 Basic Protocol 2: Synthesis of chiral bicyclic imidazole Ad-DPI Basic Protocol 3: Synthesis of remdesivir.
抗covid -19药物瑞德西韦的化学合成。
瑞德西韦已成为治疗COVID-19的重要复方药物。在这里，我们描述了这种抗covid -19药物的催化不对称合成。首先，用简单的方法合成了对外消旋磷酰氯。然后，通过手性双环咪唑催化p -外消旋氯磷对受保护核苷GS441524的有机催化不对称磷酸化，可以得到受保护的瑞德西韦。最后，瑞德西韦很容易通过去保护制备。©2021 Wiley期刊有限责任公司基本方案1:合成2-乙基丁基(氯(苯氧基)磷酰基)- l -丙氨酸丙酸酯rac-4基本方案2:合成手性双环咪唑Ad-DPI基本方案3:合成瑞德西韦。
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